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Department of Pharmacology, East Carolina University School of Medicine, Greenville, NC 27858, USA. ncozzi@brody.med.ecu.edu

Methcathinone and methylone, the beta-ketone analogues of methamphetamine and 3,4-methylenedioxymethamphetamine (MDMA), respectively, were tested for neurotransmitter uptake inhibition in vitro. The beta-ketones were threefold less potent than the nonketo drugs at inhibiting platelet serotonin accumulation, with IC(50)'s of 34.6+/-4.8 microM and 5.8+/-0.7 microM, respectively. Methcathinone and methylone were similar in potency to methamphetamine and MDMA at catecholamine transporters individually expressed in transfected glial cells. For dopamine uptake, IC(50)'s were 0.36+/-0.06 microM and 0.82+/-0.17 microM, respectively; for noradrenaline uptake, IC(50) values were 0.51+/-0.10 microM and 1. 2+/-0.1 microM, respectively. In chromaffin granules, IC(50)'s for serotonin accumulation were 112+/-8.0 microM for methcathinone and 166+/-12 microM for methylone, 10-fold higher than the respective values for methamphetamine and MDMA. Our results indicate that methcathinone and methylone potently inhibit plasma membrane catecholamine transporters but only weakly inhibit the vesicle transporter.

Methcathinone, the benzylic ketone analog of methamphetamine (MA), and methylone, the benzylic ketone analog of 3,4-methylenedioxymethamphetamine (MDMA), were synthesized and tested for their abilities to inhibit monoamine uptake in vitro. Methcathinone and methylone were threefold less potent than MA or MDMA at inhibiting [<SUP>3</SUP>H]5-HT uptake into human platelets, with IC<SUB>50</SUB>'s of 31.4 ± 7.3 mM and 5.8 ± 0.7 mM, respectively. In C6 glial cells stably expressing the rat dopamine transporter, methcathinone and methylone were similar in potency to MA and MDMA, with IC<SUB>50</SUB>'s for [<SUP>3</SUP>H]DA uptake of 0.36 ± 0.06 mM and 0.82 ± 0.17 mM, respectively. Methcathinone and methylone were also similar in potency to MA and MDMA in C6 cells expressing the human norepinephrine transporter, with IC<SUB>50</SUB>'s for [<SUP>3</SUP>H]NE accumulation of 0.51 ± 0.10 mM and 1.2 ± 0.1 mM, respectively. The benzylic ketone moiety of methcathinone and methylone had a large (tenfold) negative impact on the abilities of these drugs to inhibit the vesicular monoamine transporter (VMAT2) compared to MA and MDMA. In VMAT2-containing bovine chromaffin granules, the IC<SUB>50</SUB>'s for [<SUP>3</SUP>H]5-HT uptake were 103 ± 15 mM for methcathinone and 125 ± 16 mM for methylone. These results indicate that methcathinone and methylone are potent and selective inhibitors of plasma membrane catecholamine reuptake transporters, with more modest effects at the serotonin reuptake transporter. These drugs are essentially inactive at the vesicular monoamine transporter.

The benzylic ketone analogs of the psychoactive phenylisopropylamine methamphetamine (MA), MCAT, and of 3,4-methylenedioxymethamphetamine (MDMA), MDMCAT, were synthesized and compared to the nonketo compounds for their abilities to inhibit reuptake transporter-mediated [<SUP>3</SUP>H]serotonin accumulation into human platelets. MCAT inhibited [<SUP>3</SUP>H]serotonin uptake into platelets with an IC<SUB>50</SUB> of 33.7 ± 9.0 mM while MA exhibited an IC<SUB>50</SUB> of 11.7 ± 1.0 mM; this difference was not significant. The methylenedioxy-substituted compounds were about 6-fold more potent (p &lt; 0.05) than the unsubstituted compounds in this assay; MDMCAT displayed an IC<SUB>50</SUB> of 5.8 ± 0.7 mM and MDMA had an IC<SUB>50</SUB> of 2.1 ± 0.3 mM. The difference in potency between MDMCAT and MDMA was significant at p &lt; 0.01. These results indicate that beta-keto derivatization of psychoactive phenylalkylamines does not have a major impact on the drugs' ablility to inhibit serotonin uptake and that phenyl ring substitutions can enhance potency.

Not completely or fully accurate dumbdown, but easier to understand: Methylone and Methcathinone are treefold less potent than MDMA and Meth in serotonine reuptake inhibition. Simular in potency in catecholamine, adrenalineand dopamine reuptake inhibition. Thus phenyl ring substitutions are more potent in serotonine reuptake inhibition, then ketones.

It may also explain why methcathinone and methylone have dosage ranges of roughly 3 times as high then mdma and MA.Edited by: Alfa

Ok, I see now. So basically this helps support the 5ht (I think, this is off the top of my head) receptor theory for how these things work? Also good to know just cause of the possibility of other similar substitutions reacting similarly. THANKS!

With what alfa says ^^above^^ if you wanted to try and take enough methylone to produce the same serotonin 'type'effects as mdma you would be putting much more strain on your heart and dopamine system? What exactly are the effects from catecholamine reuptake inhibition?

Methylone isn't a well researched chemical (like most rc's, including the one you are in love with) so you are always taking chances. Then again look at the guy who came up with these substances, Dr Shulgin, he's 79 i think and still going strong! If you don't take stuff all the time and do your research you'll be fine *not a guarantee* If you do a search there are plenty of posts on the forum, have fun!

Oh and someone on this site evaporated the liquid off 'explosion' and it yielded 240mg of powder, so its prolly somewhere in between 240-280mg.

In my experiencemethylone doesn't give as much of a comedown as mdma, but thats just me, there are others who think its just as bad.Edited by: Iggypoop

However, I don't see any reference to Methylone. Is "Cathinone" a.k.a. Methylone? The more that I read the article, the more "Cathinone" started sounding like Methylone. Nonetheless, it never mentions the actual "Methylone" name, just Cathinone.

Methylone is not cathinone. As radiometer says it is 3,4-methylenedioxymethcathinone.Methylone(MDMC) relates to cathinone in the same way that MDMA relates to Amphetamine. MDMA, MDMC? Makes me wonder about MDMB. Did I miss something? lol. Edited by: Alfa